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1. (WO2018035079) HUMAN GHRELIN O-ACYL TRANSFERASE INHIBITORS
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Pub. No.: WO/2018/035079 International Application No.: PCT/US2017/046863
Publication Date: 22.02.2018 International Filing Date: 15.08.2017
IPC:
A61K 31/56 (2006.01) ,A61K 31/565 (2006.01) ,C07J 41/00 (2006.01) ,C07J 51/00 (2006.01)
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
A HUMAN NECESSITIES
61
MEDICAL OR VETERINARY SCIENCE; HYGIENE
K
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31
Medicinal preparations containing organic active ingredients
56
Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
565
not substituted in position 17 beta by a carbon atom, e.g. oestrane, oestradiol
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
41
Normal steroids containing one or more nitrogen atoms not belonging to a hetero ring
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
J
STEROIDS
51
Normal steroids with unmodified cyclopenta[a]hydrophenanthrene skeleton not provided for in groups C07J1/-C07J43/151
Applicants:
HOUGLAND, James, L. [US/US]; US
CHISHOLM, John, D. [US/US]; US
Inventors:
HOUGLAND, James, L.; US
CHISHOLM, John, D.; US
Agent:
PRICE, Frederick, JM; US
NOTO, Joseph, M.; US
BETTINGER, Blaine; US
MCGUIRE, George, R.; US
NOCILLY, David, L.; US
Priority Data:
62/375,69916.08.2016US
Title (EN) HUMAN GHRELIN O-ACYL TRANSFERASE INHIBITORS
(FR) INHIBITEURS DE LA GHRÉLINE O-ACYL TRANSFÉRASE HUMAINE
Abstract:
(EN) A class of cyanosteroid compounds that efficiently inhibit ghrelin acylation by ghrelin O-acyltransferase. The compounds have a steroid scaffold with α,β-unsaturated ketone in the A ring position such an a-cyanoenone. Exemplary compounds include (5S,8S,9S,10S, 13S,14S)-10,13-dimethyl-3-oxo-4,5,6,7,8,9,10,11,12,13,14,15,16,17- tetradecahydro-3H-cyclopenta[a]phenanthrene-2-carbonitrile.
(FR) L'invention concerne une classe de composés cyanostéroïdes qui inhibent efficacement l'acylation de la ghréline par la ghréline O-acyltransférase. Les composés ont un squelette stéroïde avec une cétone α,β non saturée dans la position du cycle A telle qu'une a-cyanoénone. Des exemples de composés comprennent le (5S,8S,9S, 13S, 13S,14S)-10,13-diméthyl-3-oxo -4,5,6,7,8,9,10,11,12,13,14,15,16,17-tétradécahydro-3 H-cyclopenta[a]phénanthrène-2-carbonitrile.
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Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BN, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DJ, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IR, IS, JO, JP, KE, KG, KH, KN, KP, KR, KW, KZ, LA, LC, LK, LR, LS, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PA, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SA, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW
African Regional Intellectual Property Organization (ARIPO) (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, ST, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Office (AM, AZ, BY, KG, KZ, RU, TJ, TM)
European Patent Office (EPO) (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, KM, ML, MR, NE, SN, TD, TG)
Publication Language: English (EN)
Filing Language: English (EN)